Pyrazolo-pyrimidine derivatives
    3.
    发明授权
    Pyrazolo-pyrimidine derivatives 失效
    吡唑并嘧啶衍生物

    公开(公告)号:US07378417B2

    公开(公告)日:2008-05-27

    申请号:US11156974

    申请日:2005-06-20

    CPC分类号: C07D487/04

    摘要: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5 and p are as defined in the description and to pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, to the manufacture of such compounds and compositions, and to methods of treating or preventing acute and/or chronic central nervous system disorders by administering such compounds.

    摘要翻译: 本发明涉及式(I)的化合物,其中R 1,R 2,R 3,R 4, R 5和p如说明书及其药学上可接受的盐所定义,含有这些化合物的药物组合物,以及制备这些化合物和组合物,以及治疗或预防急性和/ /或通过施用这些化合物的慢性中枢神经系统疾病。

    Carbamic acid derivatives
    5.
    发明授权

    公开(公告)号:US06462198B1

    公开(公告)日:2002-10-08

    申请号:US09545622

    申请日:2000-04-10

    IPC分类号: C07D41312

    摘要: The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula  wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulas  wherein R4 and R5 signifies hydrogen, lower alkyl, lower alkoxy, cyclohexyl, lower alkyl-cyclohexyl or trifluoromethyl, with the proviso that at least one of R4 or R5 has to be hydrogen; as well as to their pharmaceutically acceptable salts. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.

    Heterocyclic vinyl ethers
    6.
    发明授权
    Heterocyclic vinyl ethers 失效
    杂环乙烯基醚

    公开(公告)号:US06248901B1

    公开(公告)日:2001-06-19

    申请号:US09304909

    申请日:1999-05-04

    IPC分类号: C07D24908

    摘要: The compounds of the formula wherein R signifies halogen or lower alkyl; n signifies 0-3; R1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkylamino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom, as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.

    摘要翻译: 化合物R表示卤素或低级烷基; n表示0-3; R1表示低级烷基; 环烷基 任选被羟基,卤素,低级烷氧基或低级烷基取代的苄基; 任选被氨基,低级烷基氨基或二 - 低级烷基氨基取代的苯甲酰基; 乙酰基或环烷基 - 羰基; 并且通过N-原子键合并且除了连接的N原子还含有1-3个N原子的芳族5元残基以及它们的药学上可接受的盐作为治疗活性物质,特别是用于控制或预防 的急性和/或慢性神经障碍。